Matrix compositions for controlled delivery of drug substances
First Claim
1. A controlled release pharmaceutical composition for oral use in the form of a coated matrix composition, the matrix composition comprisingi) a mixture of a first polymer and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200°
- C.,the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides having a molecular weight of at least about 20,000 in crystalline and/or amorphous form, or a mixture such polymers, andthe second polymer being selected from poloxamers having an HLB value of at least 18,ii) a therapeutically, prophylactically and/or diagnostically active substance, wherein the concentration of the second polymer in the matrix composition is from about 5 to about 90% w/w,the matrix composition being provided with a coating having at least one opening exposing at least one surface of said matrix, the coating comprisinga first cellulose derivative which has thermoplastic properties and which is substantially insoluble in the aqueous medium in which the composition is to be used,and at least one of;
a second cellulose derivative which is soluble or dispersible in water,a plasticizer, anda filler,wherein the active substance is released with a substantially zero order release.
7 Assignments
0 Petitions
Accused Products
Abstract
A controlled release pharmaceutical composition for oral use is provided in the form of a coated matrix composition, the matrix composition comprising i) a mixture of a first and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° C., the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides, and the second polymer being selected form block copolymer of ethylene oxide and propylene oxide including poly(ethylene-glycol-b-(DL-lactic acid-co-glycolic acid)-b-ethylene glycol (PEG-PLGA PEG), poly((DL-lactic acid-co-glycolic acid)-g-ethylene glycol) (PLGA-g-PEG), poloxamers and polyethylene oxide-polypropylene oxide (PEO-PPO), ii) a therapeutically, prophylactically and/or diagnostically active substance, the matrix composition being provided with a coating having at least one opening exposing at one surface of said matrix, wherein the active substance is released with a substantially zero order release.
-
Citations
84 Claims
-
1. A controlled release pharmaceutical composition for oral use in the form of a coated matrix composition, the matrix composition comprising
i) a mixture of a first polymer and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° - C.,
the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides having a molecular weight of at least about 20,000 in crystalline and/or amorphous form, or a mixture such polymers, and the second polymer being selected from poloxamers having an HLB value of at least 18, ii) a therapeutically, prophylactically and/or diagnostically active substance, wherein the concentration of the second polymer in the matrix composition is from about 5 to about 90% w/w, the matrix composition being provided with a coating having at least one opening exposing at least one surface of said matrix, the coating comprising a first cellulose derivative which has thermoplastic properties and which is substantially insoluble in the aqueous medium in which the composition is to be used, and at least one of; a second cellulose derivative which is soluble or dispersible in water, a plasticizer, and a filler, wherein the active substance is released with a substantially zero order release. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69)
- C.,
-
70. A controlled release pharmaceutical composition for oral use in the form of a coated matrix composition, the matrix composition comprising
(i) a mixture of a first polymer and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° - C.,
the first polymer being selected from the group consisting of polyethylene glycols and polyethylene oxides having a molecular weight of at least about 20,000 daltons in crystalline and/or amorphous form, or a mixture of such polymers, and the second polymer being selected from block copolymers of ethylene oxide and propylene oxide having an HLB value of at least 18, and (ii) a therapeutically, prophylactically and/or diagnostically active substance, wherein the concentration of the second polymer in the matrix composition is from about 5 to about 90% w/w, the matrix composition being provided with a coating which is substantially insoluble in and impermeable to body fluids during the intended release periods, the coating having at least one opening exposing one surface of said matrix, the coating comprising one or more coating polymers which can be processed by extrusion, solution, or in the form of a dispersion, the one or more coating polymers being selected from the group consisting of cellulose acetate, polyamide, polyethylene, polyethylene terephthalate, polypropylene, polyurethane, polyvinyl acetate, polyvinyl chloride, silicone rubber, latex, polyhydroxybutyrate, polyhydroxyvalerate, teflon, polylactic acid or polyglycolic acid and copolymers thereof, ethylene vinyl acetate (EVA) copolymers, styrene-butadienestyrene (SBS) copolymers and styrene-isoprene-styrene (SIS) copolymers. - View Dependent Claims (71, 72, 73, 74, 75, 76, 77, 78, 79, 80, 81, 82, 83, 84)
- C.,
Specification